CH7057288

Catalog No.S8788 Batch:S878801

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Technical Data

Formula

C32H31N3O5S
Molecular Weight 569.67 CAS No. 2095616-82-1
Solubility (25°C)* In vitro DMSO 100 mg/mL (175.54 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description CH7057288 is a potent and selective TRK inhibitor with IC50 values of 1.1 nM, 7.8 nM and 5.1 nM for TRKA, TRKB, and TRKC respectively.
Targets
TrkA [1]
(Cell-free assay)		 TrkC [1]
(Cell-free assay)		 TrkB [1]
(Cell-free assay)
1.1 nM 5.1 nM 7.8 nM
In vitro

CH7057288 shows selective inhibitory activity against TRKA, TRKB, and TRKC in cell-free kinase assays and suppresses proliferation of TRK fusion-positive cell lines, but not that of TRK-negative cell lines. CH7057288 suppresses mitogen-activated protein kinase (MAPK) and E2F pathways as downstream signaling of TRK fusion[1].
In vivo

Strong in vivo tumor growth inhibition is observed in subcutaneously implanted xenograft tumor models of TRK fusion-positive cells. Furthermore, in an intracranial implantation model mimicking brain metastasis, CH7057288 significantly induces tumor regression and improves event-free survival. CH7057288 induces potent tumor growth inhibition against all three models, with remarkable tumor regression in CUTO-3 and MO-91. CH7057288 exhibits dose-dependent exposure. Because of relatively short terminal half-life (3 to 5 hours), the plasma concentration 24 hours after dose dropped to approximately a few tenths to a hundredth of Tmax[1].

Protocol (from reference)

Cell Assay:

[1]
  • Cell lines

    The NSCLC cell line CUTO-3, CRC cell line KM12-Luc, and acute myeloid leukemia cell line MO-91 harbor MPRIP-NTRK1, TPM3-NTRK1, and ETV6-NTRK3, respectively

  • Concentrations

    0.01, 0.1 and 1 μM

  • Incubation Time

    2 h

  • Method

    TRK fusion-positive cancer cell lines CUTO-3, KM12-Luc, and MO-91 are treated with the indicated concentrations of CH7057288 for 2 hours. The cells are lysed and analyzed by western blotting.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.